Chemistry:PUGNAc
PUGNAc is a 1,5-hydroximolactone, acting as an inhibitor of a variety of N-acetylhexosaminidases.[1] It was long thought that increased levels of O-GlcNAc in human cells lead to Type II diabetes. O-GlcNAc levels were artificially raised with PUGNAc, which inhibits O-GlcNAcase, a beta-exo-N-acetylhexosaminidase which cleaves beta-O-linked-N-acetylglucosamine residues from glycoproteins. As a result of this inhibition, a type II diabetic phenotype was observed. Recent pharmacological studies using a more selective O-GlcNAcase inhibitor did not see this effect. However, genetic manipulation of O-GlcNAc levels is consistent with the effects observed by PUGNAc, namely insulin resistance upon elevation of O-GlcNAc levels.[2]
In popular culture
PUGNAc was used by Michael Scofield in the television series Prison Break to keep his blood sugar level high to appear diabetic.[3]
References
- ↑ "Chemical biology of O-GlcNAc glycosylation". Chemical biology of glycoproteins. United Kingdom: Royal Society of Chemistry. March 2017. pp. 94–149. doi:10.1039/9781782623823-00094. ISBN 978-1-78801-122-8. https://books.google.com/books?id=WmwoDwAAQBAJ&dq=PUGNAc&pg=PT102.
- ↑ "Opportunities for Therapeutic Modulation of O-GlcNAc" (in en). Chemical Reviews 124 (22): 12918–13019. 2024-11-07. doi:10.1021/acs.chemrev.4c00417. ISSN 0009-2665. PMID 39509538.
- ↑ Season 1, episode 1
Further reading
- "Elevated nucleocytoplasmic glycosylation by O-GlcNAc results in insulin resistance associated with defects in Akt activation in 3T3-L1 adipocytes". Proceedings of the National Academy of Sciences of the United States of America 99 (8): 5313–8. April 2002. doi:10.1073/pnas.072072399. PMID 11959983. Bibcode: 2002PNAS...99.5313V.
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